苯硼酸修饰的树形高分子作为高效的多肽胞内递送载体（英文）

小肽及其类似物在生命活动中发挥着至关重要的作用.开发高效、安全的小肽胞内递送技术对于生物医药以及生命科学基础研究都具有重要意义.当前,将不同性质的小肽高效递送到细胞中并使其发挥生物学功能仍然面临挑战.本文通过在树形高分子表面修饰苯硼酸基团得到一种小肽胞内递送载体.该载体可以将不同极性和带电性质的小肽高效、安全地递送到多种细胞系中.与传统的穿膜肽相比,该方法对小肽的递送效率更高,同时能够更加有效地保护小肽避免其被蛋白酶降解,维持其生物学活性.通过该研究,我们得到了一种高效、通用的小肽胞内递送方法,为小肽递送载体的理性设计提供了新的思路.

Boronic acid-rich dendrimer for efficient intracellular peptide delivery

Interests in intracellular peptide delivery have continued to grow,significantly fueled by the importance of peptides and their mimetics in modern cell biology and pharmaceutical industry.However,efficient intracellular delivery of membrane-impermeable peptides of different polarities remains a challenging task.In this study,we develop a general and robust strategy for intracellular peptide delivery by using a boronic acid-rich dendrimer.The designed material is capable of transporting peptides with different polarities and charge properties into the cytosol of various cell lines without inducing additional cytotoxicity.The transduction efficacy and proteolytic stability of cargo peptides delivered by the boronic acid-rich dendrimer are much superior to peptides conjugated with cell penetrant peptides such as octaarginine.In addition,the bioactivities of pro-apoptotic peptides are maintained after intracellular delivery.This study provides a versatile and robust platform for the intracellular delivery of membrane-impermeable peptides.